EP2800749A4 - IPA INHIBITORS - Google Patents

IPA INHIBITORS

Info

Publication number
EP2800749A4
EP2800749A4 EP13733613.7A EP13733613A EP2800749A4 EP 2800749 A4 EP2800749 A4 EP 2800749A4 EP 13733613 A EP13733613 A EP 13733613A EP 2800749 A4 EP2800749 A4 EP 2800749A4
Authority
EP
European Patent Office
Prior art keywords
ipa
inhibitors
ipa inhibitors
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP13733613.7A
Other languages
German (de)
French (fr)
Other versions
EP2800749B1 (en
EP2800749A1 (en
Inventor
Frederick Cohen
John A Flygare
Lewis J Gazzard
Vickie Hsiao-Wei Tsui
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Genentech Inc
Curis Inc
Original Assignee
Genentech Inc
Curis Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to PL16189661T priority Critical patent/PL3133073T3/en
Priority to HRP20161381TT priority patent/HRP20161381T1/en
Priority to RS20160910A priority patent/RS55327B1/en
Priority to DK16189661.8T priority patent/DK3133073T3/en
Priority to MEP-2016-235A priority patent/ME02526B/en
Priority to SI201330343A priority patent/SI2800749T1/en
Priority to EP16189661.8A priority patent/EP3133073B1/en
Application filed by Genentech Inc, Curis Inc filed Critical Genentech Inc
Publication of EP2800749A1 publication Critical patent/EP2800749A1/en
Publication of EP2800749A4 publication Critical patent/EP2800749A4/en
Application granted granted Critical
Publication of EP2800749B1 publication Critical patent/EP2800749B1/en
Priority to CY20181100652T priority patent/CY1120355T1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06—Tripeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/421—1,3-Oxazoles, e.g. pemoline, trimethadione
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0815—Tripeptides with the first amino acid being basic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
EP13733613.7A 2012-01-03 2013-01-03 Inhibitors of iap Active EP2800749B1 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
RS20160910A RS55327B1 (en) 2012-01-03 2013-01-03 IAP INHIBITORS
DK16189661.8T DK3133073T3 (en) 2012-01-03 2013-01-03 IAP inhibitors
MEP-2016-235A ME02526B (en) 2012-01-03 2013-01-03 IAP INHIBITORS
SI201330343A SI2800749T1 (en) 2012-01-03 2013-01-03 Inhibitors of iap
PL16189661T PL3133073T3 (en) 2012-01-03 2013-01-03 Inhibitors of iap
HRP20161381TT HRP20161381T1 (en) 2012-01-03 2013-01-03 Inhibitors of iap
EP16189661.8A EP3133073B1 (en) 2012-01-03 2013-01-03 Inhibitors of iap
CY20181100652T CY1120355T1 (en) 2012-01-03 2018-06-22 SUSPENSIONS TOY IAP

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261582760P 2012-01-03 2012-01-03
PCT/US2013/020124 WO2013103703A1 (en) 2012-01-03 2013-01-03 Inhibitors of iap

Related Child Applications (1)

Application Number Title Priority Date Filing Date
EP16189661.8A Division EP3133073B1 (en) 2012-01-03 2013-01-03 Inhibitors of iap

Publications (3)

Publication Number Publication Date
EP2800749A1 EP2800749A1 (en) 2014-11-12
EP2800749A4 true EP2800749A4 (en) 2015-08-05
EP2800749B1 EP2800749B1 (en) 2016-09-21

Family

ID=48695302

Family Applications (2)

Application Number Title Priority Date Filing Date
EP13733613.7A Active EP2800749B1 (en) 2012-01-03 2013-01-03 Inhibitors of iap
EP16189661.8A Active EP3133073B1 (en) 2012-01-03 2013-01-03 Inhibitors of iap

Family Applications After (1)

Application Number Title Priority Date Filing Date
EP16189661.8A Active EP3133073B1 (en) 2012-01-03 2013-01-03 Inhibitors of iap

Country Status (41)

Country Link
US (6) US8716236B2 (en)
EP (2) EP2800749B1 (en)
JP (2) JP5747137B2 (en)
KR (3) KR101855566B1 (en)
CN (2) CN104159897A (en)
AR (2) AR089623A1 (en)
AU (1) AU2013202780B2 (en)
BR (1) BR112014016637B1 (en)
CA (1) CA2861637C (en)
CL (1) CL2014001770A1 (en)
CO (1) CO7020915A2 (en)
CR (1) CR20140367A (en)
CY (2) CY1118371T1 (en)
DK (2) DK2800749T3 (en)
EC (1) ECSP14011792A (en)
ES (2) ES2672809T3 (en)
HK (1) HK1203949A1 (en)
HR (2) HRP20161381T1 (en)
HU (2) HUE037760T2 (en)
IL (2) IL242314A (en)
LT (2) LT2800749T (en)
MA (1) MA35895B1 (en)
ME (2) ME02526B (en)
MX (1) MX336294B (en)
MY (1) MY178390A (en)
NO (1) NO2755614T3 (en)
NZ (1) NZ627480A (en)
PE (1) PE20142182A1 (en)
PH (2) PH12014501534B1 (en)
PL (2) PL3133073T3 (en)
PT (2) PT2800749T (en)
RS (2) RS57438B1 (en)
RU (2) RU2728789C2 (en)
SG (1) SG11201403784QA (en)
SI (2) SI3133073T1 (en)
SM (2) SMT201800352T1 (en)
TR (1) TR201808088T4 (en)
TW (1) TWI503318B (en)
UA (1) UA114417C2 (en)
WO (1) WO2013103703A1 (en)
ZA (1) ZA201405535B (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO2755614T3 (en) 2012-01-03 2018-03-31
WO2016079527A1 (en) 2014-11-19 2016-05-26 Tetralogic Birinapant Uk Ltd Combination therapy
WO2016097773A1 (en) 2014-12-19 2016-06-23 Children's Cancer Institute Therapeutic iap antagonists for treating proliferative disorders
CN109705191B (en) * 2017-10-25 2022-04-29 广东东阳光药业有限公司 IAP inhibitors and their use in medicine
KR102707188B1 (en) 2017-11-13 2024-09-13 치아타이 티안큉 파마수티컬 그룹 주식회사 SMAC mimetics useful as IAP inhibitors and their uses
JP7515175B2 (en) 2018-07-31 2024-07-12 ファイメクス株式会社 Heterocyclic compounds
JP7764027B2 (en) 2019-07-31 2025-11-05 ファイメクス株式会社 heterocyclic compounds
WO2021110011A1 (en) * 2019-12-02 2021-06-10 Ascentage Pharma (Suzhou) Co., Ltd. Combination of iap inhibitors and parp or mek inhibitors or other chemotherapeutic agents
JP2023510426A (en) 2020-01-20 2023-03-13 アストラゼネカ・アクチエボラーグ Epidermal growth factor receptor tyrosine kinase inhibitors for treating cancer
CA3234317A1 (en) 2021-10-22 2023-12-14 Wa Xian Methods and compositions for treating chronic inflammatory injury, metaplasia, dysplasia and cancers of epithelial tissues
CN117110469B (en) * 2023-08-18 2025-12-09 中国检验检疫科学研究院 Method for determining forbidden components in anti-hair loss cosmetics

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060014700A1 (en) * 2004-07-02 2006-01-19 Genentech, Inc. Inhibitors of IAP

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4526988A (en) 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
JP2001521522A (en) 1997-04-15 2001-11-06 ジェネンテック，インコーポレーテッド Novel halo-alkoxycarbonyl prodrug
ES2349110T5 (en) * 2004-12-20 2013-11-27 Genentech, Inc. IAP inhibitors derived from pyrrolidine
JP5190062B2 (en) 2006-10-12 2013-04-24 ノバルティス アーゲー Pyrrolidine derivatives as IAP inhibitors
AU2008245447C1 (en) 2007-04-30 2014-11-20 Genentech, Inc. Inhibitors of IAP
NO2755614T3 (en) 2012-01-03 2018-03-31
USD690416S1 (en) 2012-12-12 2013-09-24 Pharmajet, Inc. Needle-free syringe

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060014700A1 (en) * 2004-07-02 2006-01-19 Genentech, Inc. Inhibitors of IAP

Also Published As

Publication number Publication date
HUE037760T2 (en) 2018-09-28
CN107915728B (en) 2021-04-30
CA2861637A1 (en) 2013-07-11
LT3133073T (en) 2018-06-25
EP2800749B1 (en) 2016-09-21
CN104159897A (en) 2014-11-19
PT3133073T (en) 2018-06-18
MA35895B1 (en) 2014-12-01
AR089623A1 (en) 2014-09-03
SMT201600357B (en) 2016-11-10
BR112014016637A2 (en) 2017-06-13
RU2593259C2 (en) 2016-08-10
HUE031305T2 (en) 2017-07-28
WO2013103703A1 (en) 2013-07-11
EP3133073A2 (en) 2017-02-22
MY178390A (en) 2020-10-12
CO7020915A2 (en) 2014-08-11
SI2800749T1 (en) 2016-11-30
KR20140107670A (en) 2014-09-04
HRP20180976T1 (en) 2018-08-10
EP3133073A3 (en) 2017-03-22
AR123542A2 (en) 2022-12-14
RU2014130171A (en) 2016-02-27
SMT201800352T1 (en) 2018-09-13
CN107915728A (en) 2018-04-17
TW201333001A (en) 2013-08-16
MX336294B (en) 2016-01-14
US20160102119A1 (en) 2016-04-14
ECSP14011792A (en) 2015-12-31
PH12015501038B1 (en) 2015-09-21
PL3133073T3 (en) 2018-09-28
ES2672809T3 (en) 2018-06-18
CA2861637C (en) 2017-07-18
CR20140367A (en) 2015-02-18
RU2016124658A3 (en) 2019-09-09
JP5747137B2 (en) 2015-07-08
HRP20161381T1 (en) 2016-12-02
RU2728789C2 (en) 2020-07-31
US9586991B2 (en) 2017-03-07
US20220211797A1 (en) 2022-07-07
AU2013202780A1 (en) 2013-07-18
RU2016124658A (en) 2018-12-04
BR112014016637B1 (en) 2022-06-14
US20130172264A1 (en) 2013-07-04
US9238675B2 (en) 2016-01-19
DK2800749T3 (en) 2016-11-07
MX2014007895A (en) 2015-03-19
JP2015504072A (en) 2015-02-05
SG11201403784QA (en) 2014-08-28
US20140235551A1 (en) 2014-08-21
PT2800749T (en) 2016-10-24
JP2015199738A (en) 2015-11-12
KR20180051646A (en) 2018-05-16
NO2755614T3 (en) 2018-03-31
PH12014501534A1 (en) 2014-10-08
KR101855566B1 (en) 2018-05-04
PH12015501038A1 (en) 2015-09-21
TWI503318B (en) 2015-10-11
PE20142182A1 (en) 2015-01-16
NZ627480A (en) 2016-04-29
KR101553792B1 (en) 2015-09-16
ME03084B (en) 2019-01-20
US20190224269A1 (en) 2019-07-25
TR201808088T4 (en) 2018-06-21
PH12014501534B1 (en) 2014-10-08
DK3133073T3 (en) 2018-06-18
US8716236B2 (en) 2014-05-06
KR20150065960A (en) 2015-06-15
US20170136084A1 (en) 2017-05-18
CY1118371T1 (en) 2017-06-28
CY1120355T1 (en) 2019-07-10
BR112014016637A8 (en) 2017-07-04
AU2013202780B2 (en) 2015-04-16
SI3133073T1 (en) 2018-06-29
HK1203949A1 (en) 2015-11-06
KR101917992B1 (en) 2018-11-13
EP3133073B1 (en) 2018-05-02
US11096982B2 (en) 2021-08-24
EP2800749A1 (en) 2014-11-12
ZA201405535B (en) 2017-08-30
ME02526B (en) 2017-02-20
CL2014001770A1 (en) 2015-04-17
IL233386A (en) 2016-08-31
US11963994B2 (en) 2024-04-23
RS57438B1 (en) 2018-09-28
IL233386A0 (en) 2014-08-31
ES2594856T3 (en) 2016-12-23
RS55327B1 (en) 2017-03-31
IL242314A (en) 2016-08-31
LT2800749T (en) 2016-10-25
PL2800749T3 (en) 2017-01-31
UA114417C2 (en) 2017-06-12

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